TY - JOUR
T1 - A comparison of in vivo and in vitro metabolites of the h1-antagonist n, n-dimethyl-n'-2-pyridyl-n'-(2-thienylmethyl)- 1,2-ethanediamine (methapyrilene) in the rat
AU - Singer, S. S.
AU - Lijinsky, W.
AU - Kratz, L. E.
AU - Jr, N. Castagnoli
AU - Rose, J. E.
N1 - Funding Information:
Research sponsored by the National Cancer Institute, DHSS, under contract No. N01-CO-23909 with Bionetics Research, Inc. and by NIH training grant no. GM07175. The contents of this publication do not necessarily reflect the views or policies of the Department of Health and Human Services, nor does mention of tradenames, commercial products, or organizations imply endorsement by the US Government.
PY - 1987
Y1 - 1987
N2 - 1. The H1-antagonist N, N-dimethyl-N'-2-pyridyl-N'-(2-thienylmethyl)- 1,2-ethanediamine (methapyrilene) is carcinogenic in rats. 2. The compound, which is inactive in short-term tests and does not bind to DNA, has been classified as a non-genotoxic carcinogen. 3. Studies have been made in vitro and in vivo in F344 and Sprague-Dawley rats. New metabolites include N-(N',N'-dimethylaminoethyl)-2-aminopyridine and the corresponding N'-oxide, a derivative in which methapyrilene is hydroxylated on the 5-position of the pyridine ring, 2-(N',N'-dimethylamino)-N-2'pyridylacetamide, N-(2-pyridyl)-N-2'thienylmethyl)aminoacetaldehyde, and 2-hydroxymethylthiophene. 4. Both strains of rat metabolize methapyrilene to reactive species which may be of importance in the carcinogenic process.
AB - 1. The H1-antagonist N, N-dimethyl-N'-2-pyridyl-N'-(2-thienylmethyl)- 1,2-ethanediamine (methapyrilene) is carcinogenic in rats. 2. The compound, which is inactive in short-term tests and does not bind to DNA, has been classified as a non-genotoxic carcinogen. 3. Studies have been made in vitro and in vivo in F344 and Sprague-Dawley rats. New metabolites include N-(N',N'-dimethylaminoethyl)-2-aminopyridine and the corresponding N'-oxide, a derivative in which methapyrilene is hydroxylated on the 5-position of the pyridine ring, 2-(N',N'-dimethylamino)-N-2'pyridylacetamide, N-(2-pyridyl)-N-2'thienylmethyl)aminoacetaldehyde, and 2-hydroxymethylthiophene. 4. Both strains of rat metabolize methapyrilene to reactive species which may be of importance in the carcinogenic process.
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U2 - 10.3109/00498258709047159
DO - 10.3109/00498258709047159
M3 - Article
C2 - 3433800
AN - SCOPUS:0023636022
SN - 0049-8254
VL - 17
SP - 1279
EP - 1291
JO - Xenobiotica
JF - Xenobiotica
IS - 11
ER -